It is known in the art to employ organic compounds as antihypertensive agents and/or as agents for the treatment of cognitive and related neural behavioral problems in mammals.
Dusza et al., U.S. Pat. No. 4,236,005 disclose substituted pyrazolo(1,5-a) pyrimidines (I) and imidazo (1,5-a) pyrimidine (II) compounds of the formulae: ##STR1## wherein R.sub.1 is hydrogen or alkyl having from 1 to 3 carbon atoms; R.sub.2 is selected from the group consisting of phenyl, ortho-trifluoromethylphenyl, meta-trifluoromethylphenyl and meta-methoxyphenyl; R.sub.3 is hydrogen, fluoro, chloro, bromo, cyano, cyanomethyl, carbamoyl or alkyl having from 1 to 3 carbon atoms; and R.sub.4 is selected from the group consisting of hydrogen, fluoro, chloro, bromo, formyl, carboxyl, cyano, hydroxymethyl, N-hydroxyformimidoyl, alkyl having from 1 to 3 carbon atoms, ##STR2## wherein R is alkyl having from 1 to 3 carbon atoms; which possess central nervous system activity and are useful as anxiolytic agents.
Dusza, et al., U.S. Pat. No. 4,281,000, disclose pyrazolo(1,5-a)pyrimidine compounds of the formula: ##STR3## wherein R.sub.1 is hydrogen or alkyl having from 1 to 3 carbon atoms; R.sub.2 is selected from the group consisting of ##STR4## wherein R' is hydrogen or alkyl having from 1 to 3 carbon atoms; R.sub.3 is hydrogen, fluoro, chloro, bromo, cyano, cyanomethyl, carbamoyl or alkyl having from 1 to 3 carbon atoms; R.sub.4 is selected from the group consisting of hydrogen, fluoro, chloro, bromo, formyl, carboxyl, cyano, hydroxymethyl, N-hydroxyformimidoyl, alkyl having from 1 to 3 carbon atoms, ##STR5## wherein R is alkyl having from 1 to 3 carbon atoms; which possess anxiolytic activity.
Dusza et al., U.S. Pat. No. 4,178,449 describe substituted pyrazolo(1,5-a) pyrimidines and imidazo(1,5-a) pyrimidines of the formula ##STR6## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in relation to formulae (I) and (II); which possess anxiolytic activity.
Epstein et al., U.S. Pat. application Ser. No. 07/278,296, filed Nov. 30, 1988, now allowed, disclose compounds of the formula ##STR7## wherein R.sub.1 and R.sub.2 are each individually selected from the group consisting of hydrogn, alkyl (C.sub.1 -C.sub.4), benzoyl, mono or dissubstituted benzoyl wherein the substituents are alkyl (C.sub.1 -C.sub.6), alkoxy (C.sub.1 -C.sub.6), acyloxy (C.sub.2 -C.sub.7), halogen, nitro or trifluoromethyl, and moieties of the formulae ##STR8## wherein n is an integer from 1 to 3 and R is hydroxy, 4-morpholinyl, 1H-imidazol-1-yl, --CH(alkoxy(C.sub.1 -C.sub.3)).sub.2, .alpha.-hydroxybenzyl, phenyl or mono or disubstituted phenyl wherein the substitutents are halogen or alkyl (C.sub.1 -C.sub.6); R.sub.1 and R.sub.2 taken together with their associated nitrogen is 4-morpholinyl or a moiety of the formula --N(CH.sub.2)m wherein m is an integer of 2 to 6; R.sub.3 is hydrogen or alkyl (C.sub.1 -C.sub.6) R.sub.4 is hydrogen, halogen, alkoxy (C.sub.1 -C.sub.3), alkyl (C.sub.1 -C.sub.3) or trifluoromethyl; and R.sub.5 is hydrogen or alkyl (C.sub.1 -C.sub.6); which are useful in the treatment of cognitive and related neural behavioral disorders in warm blooded animals.
Francis et al. U.S. Pat. No. 4,713,387 disclose triazoloquinazoline compounds of the formula ##STR9## wherein R.sub.1 is optionaly substituted phenyl, pyridyl, furyl thienyl, dihydro or tetrahydrofuranyl or thienyl, pyranyl, or O-ribofuranosyl; R.sub.2 is hydrogen or lower alkyl; X is oxygen, sulfur or NR.sub.3 where R.sub.3 is hydrogen, lower alkyl, aryl-lower alkyl, cycloalkyl, lower alkenyl in which the unsaturated bond is separated from the nitrogen atom by at least one saturated carbon atom, lower alkynyl in which the unsaturated bond is separated from the nitrogen by at least one saturated carbon atom, aryl, amino-lower alkyl, lower alkylamino-lower alkyl, di-lower alkylamino-lower alkyl or hydroxy-lower alkyl; and Ring A is unsubstituted or substituted by lower alkyl, lower alkoxy, hydroxy, halogen, trifluoromethyl, nitro, amino, lower alkyl thio, lower alkyl sulfonyl, lower alkyl sulfinyl or aryl-lower alkoxy; which are useful as adenosine antagonists and benzodiazepine antagonists.
Also to be mentioned is Hamilton et al., U.S. Pat. No. 4,614,732 which discloses N.sup.6 -acenaphthyl adenosines and analogs thereof useful in lowering blood pressure in mammals.
None of the above patents disclose the novel 2,4,8-trisubstituted-3H,6H-1,4,5a,8a-tetraazaacenaphthylene-3,5-(4H)diones and 2,4,8-trisubstituted-4,5-dihydro-5-thioxo-3H,6H-1,4,5a,8a-tetraazaacenapht hylene-3-ones of the present invention. Surprisingly the dione compounds of the present invention possess anti-hypertensive activity and are useful as agents in the treatment of cognitive and related neural behavioral problems in mammals; and the 5-thioxo compounds are useful as intermediates and in the treatment of cognitive and related neural behavioral problems in mammals.